Apoptosis
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As one of the cellular death mechanisms, apoptosis, also known as programmed cell death, can be defined as the process of a proper death of any cell under certain or necessary conditions. Apoptosis is controlled by the interactions between several molecules and responsible for the elimination of unwanted cells from the body.
Many biochemical events and a series of morphological changes occur at the early stage and increasingly continue till the end of apoptosis process. Morphological event cascade including cytoplasmic filament aggregation, nuclear condensation, cellular fragmentation, and plasma membrane blebbing finally results in the formation of apoptotic bodies. Several biochemical changes such as protein modifications/degradations, DNA and chromatin deteriorations, and synthesis of cell surface markers form morphological process during apoptosis.
Apoptosis can be stimulated by two different pathways: (1) intrinsic pathway (or mitochondria pathway) that mainly occurs via release of cytochrome c from the mitochondria and (2) extrinsic pathway when Fas death receptor is activated by a signal coming from the outside of the cell.
Different gene families such as caspases, inhibitor of apoptosis proteins, B cell lymphoma (Bcl)-2 family, tumor necrosis factor (TNF) receptor gene superfamily, or p53 gene are involved and/or collaborate in the process of apoptosis.
Caspase family comprises conserved cysteine aspartic-specific proteases, and members of caspase family are considerably crucial in the regulation of apoptosis. There are 14 different caspases in mammals, and they are basically classified as the initiators including caspase-2, -8, -9, and -10; and the effectors including caspase-3, -6, -7, and -14; and also the cytokine activators including caspase-1, -4, -5, -11, -12, and -13. In vertebrates, caspase-dependent apoptosis occurs through two main interconnected pathways which are intrinsic and extrinsic pathways. The intrinsic or mitochondrial apoptosis pathway can be activated through various cellular stresses that lead to cytochrome c release from the mitochondria and the formation of the apoptosome, comprised of APAF1, cytochrome c, ATP, and caspase-9, resulting in the activation of caspase-9. Active caspase-9 then initiates apoptosis by cleaving and thereby activating executioner caspases. The extrinsic apoptosis pathway is activated through the binding of a ligand to a death receptor, which in turn leads, with the help of the adapter proteins (FADD/TRADD), to recruitment, dimerization, and activation of caspase-8 (or 10). Active caspase-8 (or 10) then either initiates apoptosis directly by cleaving and thereby activating executioner caspase (-3, -6, -7), or activates the intrinsic apoptotic pathway through cleavage of BID to induce efficient cell death. In a heat shock-induced death, caspase-2 induces apoptosis via cleavage of Bid.
Bcl-2 family members are divided into three subfamilies including (i) pro-survival subfamily members (Bcl-2, Bcl-xl, Bcl-W, MCL1, and BFL1/A1), (ii) BH3-only subfamily members (Bad, Bim, Noxa, and Puma9), and (iii) pro-apoptotic mediator subfamily members (Bax and Bak). Following activation of the intrinsic pathway by cellular stress, pro‑apoptotic BCL‑2 homology 3 (BH3)‑only proteins inhibit the anti‑apoptotic proteins Bcl‑2, Bcl-xl, Bcl‑W and MCL1. The subsequent activation and oligomerization of the Bak and Bax result in mitochondrial outer membrane permeabilization (MOMP). This results in the release of cytochrome c and SMAC from the mitochondria. Cytochrome c forms a complex with caspase-9 and APAF1, which leads to the activation of caspase-9. Caspase-9 then activates caspase-3 and caspase-7, resulting in cell death. Inhibition of this process by anti‑apoptotic Bcl‑2 proteins occurs via sequestration of pro‑apoptotic proteins through binding to their BH3 motifs.
One of the most important ways of triggering apoptosis is mediated through death receptors (DRs), which are classified in TNF superfamily. There exist six DRs: DR1 (also called TNFR1); DR2 (also called Fas); DR3, to which VEGI binds; DR4 and DR5, to which TRAIL binds; and DR6, no ligand has yet been identified that binds to DR6. The induction of apoptosis by TNF ligands is initiated by binding to their specific DRs, such as TNFα/TNFR1, FasL /Fas (CD95, DR2), TRAIL (Apo2L)/DR4 (TRAIL-R1) or DR5 (TRAIL-R2). When TNF-α binds to TNFR1, it recruits a protein called TNFR-associated death domain (TRADD) through its death domain (DD). TRADD then recruits a protein called Fas-associated protein with death domain (FADD), which then sequentially activates caspase-8 and caspase-3, and thus apoptosis. Alternatively, TNF-α can activate mitochondria to sequentially release ROS, cytochrome c, and Bax, leading to activation of caspase-9 and caspase-3 and thus apoptosis. Some of the miRNAs can inhibit apoptosis by targeting the death-receptor pathway including miR-21, miR-24, and miR-200c.
p53 has the ability to activate intrinsic and extrinsic pathways of apoptosis by inducing transcription of several proteins like Puma, Bid, Bax, TRAIL-R2, and CD95.
Some inhibitors of apoptosis proteins (IAPs) can inhibit apoptosis indirectly (such as cIAP1/BIRC2, cIAP2/BIRC3) or inhibit caspase directly, such as XIAP/BIRC4 (inhibits caspase-3, -7, -9), and Bruce/BIRC6 (inhibits caspase-3, -6, -7, -8, -9).
Any alterations or abnormalities occurring in apoptotic processes contribute to development of human diseases and malignancies especially cancer.
References:
1.Yağmur Kiraz, Aysun Adan, Melis Kartal Yandim, et al. Major apoptotic mechanisms and genes involved in apoptosis[J]. Tumor Biology, 2016, 37(7):8471.
2.Aggarwal B B, Gupta S C, Kim J H. Historical perspectives on tumor necrosis factor and its superfamily: 25 years later, a golden journey.[J]. Blood, 2012, 119(3):651.
3.Ashkenazi A, Fairbrother W J, Leverson J D, et al. From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors[J]. Nature Reviews Drug Discovery, 2017.
4.McIlwain D R, Berger T, Mak T W. Caspase functions in cell death and disease[J]. Cold Spring Harbor perspectives in biology, 2013, 5(4): a008656.
5.Ola M S, Nawaz M, Ahsan H. Role of Bcl-2 family proteins and caspases in the regulation of apoptosis[J]. Molecular and cellular biochemistry, 2011, 351(1-2): 41-58.
Research Areas
- Caspase(114)
- Pyroptosis(37)
- 14.3.3 Proteins(1)
- Apoptosis Inducers(42)
- Bax(6)
- Bcl-2 Family(154)
- Bcl-xL(8)
- c-RET(8)
- IAP(31)
- KEAP1-Nrf2(81)
- MDM2(12)
- p53(145)
- PC-PLC(4)
- PKD(6)
- RasGAP (Ras- P21)(1)
- Survivin(12)
- Thymidylate Synthase(10)
- TNF-α(189)
- Other Apoptosis(877)
- APC(6)
- PD-1/PD-L1 interaction(106)
- ASK1(4)
- PAR4(2)
- RIP kinase(55)
- FKBP(23)
- Cuproptosis(4)
Products Related to Apoptosis(3030)
- GN10535Cucurbitacin BCAS: 6199-67-3Purity: >98.00%
Cucurbitacin B is a kind of tetracyclic triterpenoid compounds isolated from cucurbitaceae, and exhibits a wide range of biological activities.
- GN10544Ginsenoside Rg1CAS: 22427-39-0Purity: >98.00%
ギンセノシドRg1(Ginsenoside Rg1)はオタネニンジンの中の主な有効成分の一種であり、ステロイド系配糖体として知られる天然物質の一種であり、広い範囲の生物学的活性を持っている。
- GN10547β-SitosterolCAS: 83-46-5Purity: >98.00%
β-Sitosterolは植物に由来する天然のステロールであり、癌の進行を阻害するなど、様々な生物活性を持っている。β-Sitosterolもよく、心血管健康における影響の研究に使われる。
- GN10561astragalinCAS: 480-10-4Purity: >98.00%
Astragalinは強い抗酸化と抗炎症活性を持つ天然のフラボノイド化合物であり、癌や心血管疾患など様々な疾患では強力な治療応用力を示している。
- GN10585TetramethylpyrazineCAS: 1124-11-4Purity: >99.50%
Tetramethylpyrazineはセンキュウから単離されたアルカロイドであり、抗炎症、抗酸化、抗腫瘍、オートファジー調節、血管拡張、血管新生調節、ミトコンドリア損傷抑制、内皮保護と神経保護作用を持つ。
- GN106295,7-dihydroxychromoneCAS: 31721-94-5Purity: >99.00%
5,7-dihydroxychromoneは、ピーナッツの殻由来のフラボノイド分解生成物であり、アサガオ、トウモロコシ、ピーナッツ、および小麦の胚軸伸長を阻害する。
- GN10648Rosmarinic acidCAS: 20283-92-5Purity: >98.00%
ロスマリン酸(Rosmarinic acid)は、植物における広いフェノール類のエステル化合物である。ロスマリン酸は抗ウイルス、抗菌、抗炎症、神経保護、抗癌、抗脂質過酸化、アポトーシスと抗酸化活性を有する。
- GN10702Asiatic acidCAS: 464-92-6Purity: >99.00%
Asiatic acidは五環式トリテルペノイドであり、EGFR活性を阻害し、野生型EGFRとT790M/L858R EGFRに対する値はそれぞれ0.035nMと0.348nMである。
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GN10535 | Cucurbitacin B | 6199-67-3 | >98.00% | |
Cucurbitacin B is a kind of tetracyclic triterpenoid compounds isolated from cucurbitaceae, and exhibits a wide range of biological activities. | ||||
| GN10538 | Ginsenoside Rh1 | 63223-86-9 | >98.00% | |
| GN10539 | Bergenin | 477-90-7 | >99.50% | |
| GN10543 | caudatin | 38395-02-7 | >98.00% | |
| GN10544 | Ginsenoside Rg1 | 22427-39-0 | >98.00% | |
ギンセノシドRg1(Ginsenoside Rg1)はオタネニンジンの中の主な有効成分の一種であり、ステロイド系配糖体として知られる天然物質の一種であり、広い範囲の生物学的活性を持っている。 | ||||
| GN10547 | β-Sitosterol | 83-46-5 | >98.00% | |
β-Sitosterolは植物に由来する天然のステロールであり、癌の進行を阻害するなど、様々な生物活性を持っている。β-Sitosterolもよく、心血管健康における影響の研究に使われる。 | ||||
| GN10560 | α-hederin | 27013-91-8 | >98.00% | |
| GN10561 | astragalin | 480-10-4 | >98.00% | |
Astragalinは強い抗酸化と抗炎症活性を持つ天然のフラボノイド化合物であり、癌や心血管疾患など様々な疾患では強力な治療応用力を示している。 | ||||
| GN10584 | Ginsenoside Rk1 | 494753-69-4 | >98.00% | |
| GN10585 | Tetramethylpyrazine | 1124-11-4 | >99.50% | |
Tetramethylpyrazineはセンキュウから単離されたアルカロイドであり、抗炎症、抗酸化、抗腫瘍、オートファジー調節、血管拡張、血管新生調節、ミトコンドリア損傷抑制、内皮保護と神経保護作用を持つ。 | ||||
| GN10629 | 5,7-dihydroxychromone | 31721-94-5 | >99.00% | |
5,7-dihydroxychromoneは、ピーナッツの殻由来のフラボノイド分解生成物であり、アサガオ、トウモロコシ、ピーナッツ、および小麦の胚軸伸長を阻害する。 | ||||
| GN10632 | Betulin | 473-98-3 | >98.00% | |
| GN10634 | Myricetin | 529-44-2 | >98.00% | |
Myricetinは植物によく存在する天然のフラボノイドであり、抗酸化、抗炎症と抗腫瘍活性を持ち、マイトジェン活性化タンパク質キナーゼキナーゼ(MEK1)とJB6 P+マウス表皮細胞の腫瘍性転換の新規阻害剤として機能する。 | ||||
| GN10639 | Methyl protodioscin | 54522-52-0 | >98.00% | |
| GN10645 | Jaceosidin | 18085-97-7 | >98% | |
| GN10648 | Rosmarinic acid | 20283-92-5 | >98.00% | |
ロスマリン酸(Rosmarinic acid)は、植物における広いフェノール類のエステル化合物である。ロスマリン酸は抗ウイルス、抗菌、抗炎症、神経保護、抗癌、抗脂質過酸化、アポトーシスと抗酸化活性を有する。 | ||||
| GN10650 | Ziyuglycoside II | 35286-59-0 | >98.00% | |
| GN10654 | (+)-Corynoline | 18797-79-0 | >98.00% | |
| GN10666 | Isoalantolactone | 470-17-7 | >98.00% | |
| GN10667 | Calycosin | 20575-57-9 | >98.00% | |
Calycosinは主に Astragalus membranaceus に存在する天然のイソフラボノイドであり、抗酸化、抗炎症と抗アポトーシスの特性を持っている。 | ||||
| GN10681 | Sophocarpine | 6483-15-4 | >98.00% | |
| GN10686 | Ginsenoside Rh2 | 78214-33-2 | >99.50% | |
| GN10702 | Asiatic acid | 464-92-6 | >99.00% | |
Asiatic acidは五環式トリテルペノイドであり、EGFR活性を阻害し、野生型EGFRとT790M/L858R EGFRに対する値はそれぞれ0.035nMと0.348nMである。 | ||||
| GN10709 | Polyphyllin A | 50773-41-6 | >98.00% | |
